Holshouser M H, Kolb M
J Pharm Sci. 1986 Jun;75(6):619-21. doi: 10.1002/jps.2600750621.
High yields of potential glycol metabolites of p-synephrine, epinephrine, octopamine, and normacromerine can be obtained from the readily available monosubstituted and disubstituted acetophenones. The general procedure involves alpha-bromination followed by displacement with acetate ion and reduction with lithium aluminum hydride. Yields ranged from 46 to 91%. Furthermore, the procedure minimizes some problems inherent in aromatic glycol synthesis which include dimerization and pinacol-pinacolone rearrangement.
从容易获得的单取代和二取代苯乙酮中，可以高产率地得到对-辛弗林、肾上腺素、章鱼胺和去甲异克卡林的潜在二醇代谢物。一般步骤包括α-溴化，然后用乙酸根离子取代，并用氢化铝锂还原。产率范围为46%至91%。此外，该方法最大限度地减少了芳香二醇合成中固有的一些问题，包括二聚化和平纳醇-频哪酮重排。
